De Paulis, T.; Hewlett, W. A.; Schmidt, D. E.; Mason, N. S.; Trivedi, B. L.; Ebert, M. H. published the artcile< Synthesis and 5-HT-3 receptor binding activity of 5-[125I]iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide and its 5-halogen-2-alkoxyl homologs>, Synthetic Route of 120570-05-0, the main research area is benzamide derivative serotonin receptor binding structure; azabicyclooctylbenzamide serotonin receptor binding structure; iodine labeling benzamide serotonin receptor binding; PET iodine labeled benzamide serotonin receptor; SPECT iodine labeled benzamide serotonin receptor.
(S)-5-Iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (MIZAC) was prepared from 5-iodo-2,3-dimethoxybenzoyl chloride and (S)-3-aminoquinuclidine. [125I]iodide-stannylation of its corresponding 5-tri-n-butyltin derivative gave [125I]-MIZAC at 1800 Ci/mmol. Binding of [125I]-MIZAC in rat entorhinal cortex revealed a KD of 1.37 nM. A series of racemic 2-O-alkyl derivatives of MIZAC were prepared and 5-HT-3 receptor affinities were determined by inhibition of [125I]-MIZAC binding. Optimal affinity for the receptor was obtained with small, electron-withdrawing substituents in the aromatic 5-position and with bulky substituents in the 3-position. [125I]-MIZAC is a selective radioligand useful for in vitro identification of the 5-HT-3 receptor. QSAR data suggest that potential candidates for SPECT and PET studies might be found in sterically bulky haloalkoxyl 5-chloro homologs of MIZAC.
European Journal of Medicinal Chemistrypublished new progress about 5-HT3 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Synthetic Route of 120570-05-0.
Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider